Ka morao

Apixaban ke inhibitor e khethang haholo ebile e fetoleloa morao ea Factor Xa e nang le boleng ba Ki ea 0.08 nM le 0.17 nM ho motho le mmutla, ka ho latellana[1].

Factor X, eo hape e tsejoang ka eponym Stuart-Prower factor, ke enzyme ea coagulation cascade.Factor X e sebelisoa, ka hydrolysis, ho factor Xa ka bobeli factor IX.Factor Xa is the activated form of the coagulation factorthrombokinase.Inhibiting Factor Xa e ka fana ka mokhoa o mong oa anticoagulation.Li-inhibitors tsa Direct Xa ke li-anticoagulants tse tsebahalang [2].

In vitro: Apixabanhas e bontšitse tekanyo e phahameng ea potency, selectivity, le katleho ho Factor Xa le Ki ea 0.08 nM le 0.17 nM bakeng sa Human Factor Xa le Rabbit Factor Xa, ka ho latellana [1].Apixaban e lelefatsa nako ea ho koala ha plasma e tloaelehileng ea motho ka li-concents (EC2x) tsa 3.6, 0.37, 7.4 le 0.4 μM, tse hlokehang ka ho latellana ho habeli nako ea prothrombin (PT), nako e fetotsoeng ea prothrombin (mPT), e entsoeng ka nako e itseng ea thromboplastin ( APTT) le HepTest.Ntle ho moo, Apixaban e bontšitse matla a phahameng ka ho fetisisa ho plasma ea batho le ea mmutla, empa matla a fokolang a plasma ea likhoto le lintja litlhahlobong tsa PT le APTT [3].

In vivo: Apixaban e hlahisitse pharmacokinetics e ntle ka ho fetisisa e nang le tumello e tlaase haholo (Cl: 0.02 L kg-1h-1), le palo e tlaase ea kabo (Vdss: 0.2 L / kg) ho ntja.Ntle ho moo, Apixaban e boetse e bonts'a halofo ea bophelo bo itekanetseng le T1 / 2 ea lihora tsa 5.8 le bioavailability e ntle ea molomo (F: 58%) [1].Ka har'a arteriovenous-shunt thrombosis (AVST), venous thrombosis (VT) le mefuta ea meutlanyana ea carotid arterial thrombosis (ECAT), Apixaban e hlahisitse litlamorao tsa antithrombotic ka EC50 ea 270 nM, 110 nM le 70 nM ka mokhoa o itšetlehileng ka lethal dose [3. ].Apixaban e thibelitse haholo ts'ebetso ea Xa ka IC50 ea 0.22 μM ho mmutla ex vivo[4].Ka lichimpanzi, Apixaban o ile a boela a bontša palo e nyenyane ea ho aba (Vdss: 0.17 L kg-1), tumello e tlaase ea tsamaiso (Cl: 0.018 L kg-1h-1), le bioavailability e ntle ea molomo (F: 59%) [5].

Litšupiso:
Pinto DJP, Orwat MJ, Koch S, et al.Ho sibolloa ha 1-(4-methoxyphenyl) -7-oxo-6-(4-(2-oxopiperidin-1-yl) phenyl) -4, 5, 6, 7-tetrahydro-1 H-pyrazolo [3, 4- c] pyridine-3-carboxamide (Apixaban, BMS-562247), e matla haholo, e khethang, e sebetsang hantle, le ea molomo ea bioavailable inhibitor ea mali a coagulation factor Xa[J].Journal of chemistry ea meriana, 2007, 50 (22): 5339-5356.
Sidhu P S. Direct Factor Xa Inhibitors e le Anticoagulants[J].
Wong PC, Crain EJ, Xin B, et al.Apixaban, oral, e tobileng le e khethehileng haholo ea Xa inhibitor: in vitro, antithrombotic le antihemostaticstudies[J].Journal of Thrombosis le Haemostasis, 2008, 6 (5): 820-829.
Zhang D, He K, Raghavan N, et al.Metabolism, pharmacokinetics le pharmacodynamics ea factor Xa inhibitor apixaban ka mebutlanyana[J].Journal of thrombosis le thrombolysis, 2010, 29 (1): 70-80.
He K, Luettgen JM, Zhang D, et al.Preclinical pharmacokinetics le pharmacodynamics ea apixaban, e matla le e khethang factor Xa inhibitor[J].Koranta ea Europe ea metabolism ea lithethefatsi le pharmacokinetics, 2011, 36 (3): 129-139.

Apixaban ke inhibitor e khethang haholo ebile e fetoleloa morao ea Factor Xa e nang le boleng ba Ki ea 0.08 nM le 0.17 nM ho motho le mmutla, ka ho latellana[1].

Factor X, eo hape e tsejoang ka eponym Stuart-Prower factor, ke enzyme ea coagulation cascade.Factor X e sebelisoa, ka hydrolysis, ho factor Xa ka bobeli factor IX.Factor Xa is the activated form of the coagulation factorthrombokinase.Inhibiting Factor Xa e ka fana ka mokhoa o mong oa anticoagulation.Li-inhibitors tsa Direct Xa ke li-anticoagulants tse tsebahalang [2].

In vitro: Apixabanhas e bontšitse tekanyo e phahameng ea potency, selectivity, le katleho ho Factor Xa le Ki ea 0.08 nM le 0.17 nM bakeng sa Human Factor Xa le Rabbit Factor Xa, ka ho latellana [1].Apixaban e lelefatsa nako ea ho koala ha plasma e tloaelehileng ea motho ka li-concents (EC2x) tsa 3.6, 0.37, 7.4 le 0.4 μM, tse hlokehang ka ho latellana ho habeli nako ea prothrombin (PT), nako e fetotsoeng ea prothrombin (mPT), e entsoeng ka nako e itseng ea thromboplastin ( APTT) le HepTest.Ntle ho moo, Apixaban e bontšitse matla a phahameng ka ho fetisisa ho plasma ea batho le ea mmutla, empa matla a fokolang a plasma ea likhoto le lintja litlhahlobong tsa PT le APTT [3].

In vivo: Apixaban e hlahisitse pharmacokinetics e ntle ka ho fetisisa e nang le tumello e tlaase haholo (Cl: 0.02 L kg-1h-1), le palo e tlaase ea kabo (Vdss: 0.2 L / kg) ho ntja.Ntle ho moo, Apixaban e boetse e bonts'a halofo ea bophelo bo itekanetseng le T1 / 2 ea lihora tsa 5.8 le bioavailability e ntle ea molomo (F: 58%) [1].Ka har'a arteriovenous-shunt thrombosis (AVST), venous thrombosis (VT) le mefuta ea meutlanyana ea carotid arterial thrombosis (ECAT), Apixaban e hlahisitse litlamorao tsa antithrombotic ka EC50 ea 270 nM, 110 nM le 70 nM ka mokhoa o itšetlehileng ka lethal dose [3. ].Apixaban e thibelitse haholo ts'ebetso ea Xa ka IC50 ea 0.22 μM ho mmutla ex vivo[4].Ka lichimpanzi, Apixaban o ile a boela a bontša palo e nyenyane ea ho aba (Vdss: 0.17 L kg-1), tumello e tlaase ea tsamaiso (Cl: 0.018 L kg-1h-1), le bioavailability e ntle ea molomo (F: 59%) [5].

Litšupiso:
Pinto DJP, Orwat MJ, Koch S, et al.Ho sibolloa ha 1-(4-methoxyphenyl) -7-oxo-6-(4-(2-oxopiperidin-1-yl) phenyl) -4, 5, 6, 7-tetrahydro-1 H-pyrazolo [3, 4- c] pyridine-3-carboxamide (Apixaban, BMS-562247), e matla haholo, e khethang, e sebetsang hantle, le ea molomo ea bioavailable inhibitor ea mali a coagulation factor Xa[J].Journal of chemistry ea meriana, 2007, 50 (22): 5339-5356.
Sidhu P S. Direct Factor Xa Inhibitors e le Anticoagulants[J].
Wong PC, Crain EJ, Xin B, et al.Apixaban, oral, e tobileng le e khethehileng haholo ea Xa inhibitor: in vitro, antithrombotic le antihemostaticstudies[J].Journal of Thrombosis le Haemostasis, 2008, 6 (5): 820-829.
Zhang D, He K, Raghavan N, et al.Metabolism, pharmacokinetics le pharmacodynamics ea factor Xa inhibitor apixaban ka mebutlanyana[J].Journal of thrombosis le thrombolysis, 2010, 29 (1): 70-80.
He K, Luettgen JM, Zhang D, et al.Preclinical pharmacokinetics le pharmacodynamics ea apixaban, e matla le e khethang factor Xa inhibitor[J].Koranta ea Europe ea metabolism ea lithethefatsi le pharmacokinetics, 2011, 36 (3): 129-139.

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